CN103739537B - New synthesis method of ezetimibe - Google Patents
New synthesis method of ezetimibe Download PDFInfo
- Publication number
- CN103739537B CN103739537B CN201310722140.5A CN201310722140A CN103739537B CN 103739537 B CN103739537 B CN 103739537B CN 201310722140 A CN201310722140 A CN 201310722140A CN 103739537 B CN103739537 B CN 103739537B
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- NGCHQYFXADRTDA-AATRIKPKSA-N C=C/C=C(\C=C)/F Chemical compound C=C/C=C(\C=C)/F NGCHQYFXADRTDA-AATRIKPKSA-N 0.000 description 1
- YSOQCCFIWNVPGL-VOTSOKGWSA-N CC/C(/F)=C(/C)\CC=[IH] Chemical compound CC/C(/F)=C(/C)\CC=[IH] YSOQCCFIWNVPGL-VOTSOKGWSA-N 0.000 description 1
- OLNTVTPDXPETLC-XPWALMASSA-N O[C@@H](CC[C@H]([C@@H](c(cc1)ccc1O)N1c(cc2)ccc2F)C1=O)c(cc1)ccc1F Chemical compound O[C@@H](CC[C@H]([C@@H](c(cc1)ccc1O)N1c(cc2)ccc2F)C1=O)c(cc1)ccc1F OLNTVTPDXPETLC-XPWALMASSA-N 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
- C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
- C07D205/06—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D205/08—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic System
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
- C07F7/1804—Compounds having Si-O-C linkages
Abstract
Description
Claims (1)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
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CN201310722140.5A CN103739537B (en) | 2013-12-24 | 2013-12-24 | New synthesis method of ezetimibe |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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CN201310722140.5A CN103739537B (en) | 2013-12-24 | 2013-12-24 | New synthesis method of ezetimibe |
Publications (2)
Publication Number | Publication Date |
---|---|
CN103739537A CN103739537A (en) | 2014-04-23 |
CN103739537B true CN103739537B (en) | 2015-05-20 |
Family
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Family Applications (1)
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CN201310722140.5A Active CN103739537B (en) | 2013-12-24 | 2013-12-24 | New synthesis method of ezetimibe |
Country Status (1)
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CN (1) | CN103739537B (en) |
Families Citing this family (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN105461649B (en) * | 2014-08-08 | 2019-10-22 | 浙江九洲药业股份有限公司 | A kind of Ezetimible intermediate and preparation method thereof |
CN106892851A (en) * | 2017-03-09 | 2017-06-27 | 上海华源医药科技发展有限公司 | A kind of new method for preparing Ezetimibe crystal formation I |
CN112441959A (en) * | 2020-12-07 | 2021-03-05 | 石家庄市华新药业有限责任公司 | Ezetimibe raw material medicine synthesis process |
CN114621126B (en) * | 2020-12-12 | 2023-07-25 | 重庆圣华曦药业股份有限公司 | Improved ezetimibe preparation method |
Citations (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1131416A (en) * | 1993-09-21 | 1996-09-18 | 先灵公司 | Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents |
WO1997045406A1 (en) * | 1996-05-31 | 1997-12-04 | Schering Corporation | 3-hydroxy gamma-lactone based enantioselective synthesis of azetidinones |
CN1329592A (en) * | 1998-12-07 | 2002-01-02 | 先灵公司 | Process for synthesis of beta-propanamide |
WO2007072088A1 (en) * | 2005-12-20 | 2007-06-28 | Richter Gedeon Nyrt. | Process for the production of ezetimibe and intermediates used in this proces |
CN101423511A (en) * | 2007-11-05 | 2009-05-06 | 中山奕安泰医药科技有限公司 | Ezetimible intermediate and synthetic method of ezetimible |
CN101935309A (en) * | 2009-06-29 | 2011-01-05 | 上海特化医药科技有限公司 | Method for preparing ezetimibe and intermediate thereof |
US20110046389A1 (en) * | 2008-02-25 | 2011-02-24 | Hana Stepankova | Intermediates for the preparation of (3r, 4s)-1-(4-fluorophenyl)-3-[(3s)-3-(4-fluorophenyl)-3-hydroxypropyl)]-4-(4-hydroxyphenyl)-2-azetidinone |
CN102234246A (en) * | 2010-04-23 | 2011-11-09 | 浙江华海药业股份有限公司 | Novel ezetimibe synthesis method |
WO2012004382A1 (en) * | 2010-07-09 | 2012-01-12 | Moehs Iberica S.L. | New method for preparing ezetimibe |
CN102850390A (en) * | 2011-07-01 | 2013-01-02 | 江苏豪森药业股份有限公司 | Intermediate of ezetimibe and its preparation method |
CN103102297A (en) * | 2012-09-28 | 2013-05-15 | 北京赛林泰医药技术有限公司 | Synthesis method of novel atorvastatin |
CN103450065A (en) * | 2013-07-15 | 2013-12-18 | 和鼎(南京)医药技术有限公司 | Preparation method of ezetimibe |
-
2013
- 2013-12-24 CN CN201310722140.5A patent/CN103739537B/en active Active
Patent Citations (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1131416A (en) * | 1993-09-21 | 1996-09-18 | 先灵公司 | Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents |
WO1997045406A1 (en) * | 1996-05-31 | 1997-12-04 | Schering Corporation | 3-hydroxy gamma-lactone based enantioselective synthesis of azetidinones |
CN1329592A (en) * | 1998-12-07 | 2002-01-02 | 先灵公司 | Process for synthesis of beta-propanamide |
WO2007072088A1 (en) * | 2005-12-20 | 2007-06-28 | Richter Gedeon Nyrt. | Process for the production of ezetimibe and intermediates used in this proces |
CN101423511A (en) * | 2007-11-05 | 2009-05-06 | 中山奕安泰医药科技有限公司 | Ezetimible intermediate and synthetic method of ezetimible |
US20110046389A1 (en) * | 2008-02-25 | 2011-02-24 | Hana Stepankova | Intermediates for the preparation of (3r, 4s)-1-(4-fluorophenyl)-3-[(3s)-3-(4-fluorophenyl)-3-hydroxypropyl)]-4-(4-hydroxyphenyl)-2-azetidinone |
CN101935309A (en) * | 2009-06-29 | 2011-01-05 | 上海特化医药科技有限公司 | Method for preparing ezetimibe and intermediate thereof |
CN102234246A (en) * | 2010-04-23 | 2011-11-09 | 浙江华海药业股份有限公司 | Novel ezetimibe synthesis method |
WO2012004382A1 (en) * | 2010-07-09 | 2012-01-12 | Moehs Iberica S.L. | New method for preparing ezetimibe |
CN102850390A (en) * | 2011-07-01 | 2013-01-02 | 江苏豪森药业股份有限公司 | Intermediate of ezetimibe and its preparation method |
CN103102297A (en) * | 2012-09-28 | 2013-05-15 | 北京赛林泰医药技术有限公司 | Synthesis method of novel atorvastatin |
CN103450065A (en) * | 2013-07-15 | 2013-12-18 | 和鼎(南京)医药技术有限公司 | Preparation method of ezetimibe |
Non-Patent Citations (2)
Title |
---|
Ezetimibe合成路线图解;蔡正艳,等;《中国医药工业杂志》;20040420;第35卷(第04期);第251-253页 * |
依折麦布中间体的合成工艺研究;蔡金刚,等;《精细化工中间体》;20110831;第41卷(第04期);第37-39页 * |
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CN103739537A (en) | 2014-04-23 |
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C06 | Publication | ||
PB01 | Publication | ||
C10 | Entry into substantive examination | ||
SE01 | Entry into force of request for substantive examination | ||
C14 | Grant of patent or utility model | ||
GR01 | Patent grant | ||
CB03 | Change of inventor or designer information |
Inventor after: Zhang Qingjie Inventor after: Yang Baohai Inventor after: Pan Bigao Inventor after: Fu Yong Inventor after: Chen Xingmen Inventor before: Yang Baohai Inventor before: Pan Bigao Inventor before: Fu Yong Inventor before: Chen Xingmen |
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COR | Change of bibliographic data | ||
TR01 | Transfer of patent right |
Effective date of registration: 20170527 Address after: 222200 Guanyun City, Jiangsu province Lingang Industrial Zone, the south side of the weft Road, eight Patentee after: Lianyungang Hengyun Pharmaceutical Co. Ltd. Address before: 222200 Jiangsu city of Lianyungang province Guanyun County Harbor Industrial Zone weft seven road No. 1 Patentee before: LIANYUNGANG HENGYUN MEDICAL TECHNOLOGY CO., LTD. |
|
CP01 | Change in the name or title of a patent holder | ||
CP01 | Change in the name or title of a patent holder |
Address after: 222200 Guanyun City, Jiangsu province Lingang Industrial Zone, the south side of the weft Road, eight Patentee after: Lianyungang Hengyun Pharmaceutical Co. Ltd. Address before: 222200 Guanyun City, Jiangsu province Lingang Industrial Zone, the south side of the weft Road, eight Patentee before: Lianyungang Hengyun Pharmaceutical Co. Ltd. |